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Assay Detail

CHEMBL4621667

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Functional
Antileishmanial activity against Leishmania donovani amastigotes infected in human THP1 cells incubated for 96 hrs
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania donovani
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania donovani (CHEMBL367)
Type ORGANISM
Organism Leishmania donovani

Publication

Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent <i>In Vitro</i> Antileishmanial Activity: Initial SAR and Assessment of <i>In Vivo</i> Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH.
J Med Chem (2020) 63 : 9523 -9539
PubMed 32663005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 5.75 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644333 1 7.00
CHEMBL4645906 1 6.80
CHEMBL267345 AMPHOTERICIN B 4.0 1 6.70
CHEMBL523303 1 6.50
CHEMBL4648046 1 6.30
CHEMBL3290936 1 6.30
CHEMBL4635381 1 6.20
CHEMBL4644580 1 6.00
CHEMBL4645520 1 5.90
CHEMBL4644468 1 5.90
CHEMBL4635260 1 5.80
CHEMBL4644369 1 5.70
CHEMBL522630 1 5.60
CHEMBL4648017 1 5.60
CHEMBL125 MILTEFOSINE 4.0 1 5.40
CHEMBL4634437 1 5.30
CHEMBL4648588 1 5.30
CHEMBL4648127 1 5.00
CHEMBL4639773 1 5.00
CHEMBL221027 1 4.80
CHEMBL4646679 1 4.80
CHEMBL4648421 1 4.50
CHEMBL4639444 1 -
CHEMBL4632697 1 -
CHEMBL4645383 1 -
CHEMBL4644400 1 -
CHEMBL254316 RALTEGRAVIR 4.0 1 -
CHEMBL4633833 1 -
CHEMBL4644356 1 -
CHEMBL4645046 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644333 EC50 = 100.0 nM 7.00
CHEMBL4645906 EC50 = 158.49 nM 6.80
CHEMBL267345 AMPHOTERICIN B EC50 = 199.53 nM 6.70
CHEMBL523303 EC50 = 316.23 nM 6.50
CHEMBL4648046 EC50 = 501.19 nM 6.30
CHEMBL3290936 EC50 = 501.19 nM 6.30
CHEMBL4635381 EC50 = 630.96 nM 6.20
CHEMBL4644580 EC50 = 1000.0 nM 6.00
CHEMBL4645520 EC50 = 1258.93 nM 5.90
CHEMBL4644468 EC50 = 1258.93 nM 5.90
CHEMBL4635260 EC50 = 1584.89 nM 5.80
CHEMBL4644369 EC50 = 1995.26 nM 5.70
CHEMBL522630 EC50 = 2511.89 nM 5.60
CHEMBL4648017 EC50 = 2511.89 nM 5.60
CHEMBL125 MILTEFOSINE EC50 = 3981.07 nM 5.40
CHEMBL4634437 EC50 = 5011.87 nM 5.30
CHEMBL4648588 EC50 = 5011.87 nM 5.30
CHEMBL4639773 EC50 = 10000.0 nM 5.00
CHEMBL4648127 EC50 = 10000.0 nM 5.00
CHEMBL221027 EC50 = 15848.93 nM 4.80
CHEMBL4646679 EC50 = 15848.93 nM 4.80
CHEMBL4648421 EC50 = 31622.78 nM 4.50
CHEMBL4642833 EC50 > 50118.72 nM -
CHEMBL4633980 EC50 > 50118.72 nM -
CHEMBL4632762 EC50 > 50118.72 nM -
CHEMBL4649578 EC50 > 50118.72 nM -
CHEMBL4639318 EC50 > 50118.72 nM -
CHEMBL4646137 EC50 > 50118.72 nM -
CHEMBL4645046 EC50 > 50118.72 nM -
CHEMBL4644356 EC50 > 50118.72 nM -
CHEMBL4633833 EC50 > 50118.72 nM -
CHEMBL254316 RALTEGRAVIR EC50 > 50118.72 nM -
CHEMBL4644400 EC50 > 50118.72 nM -
CHEMBL4645383 EC50 > 50118.72 nM -
CHEMBL4632697 EC50 > 50118.72 nM -
CHEMBL4639444 EC50 > 50118.72 nM -